长春胺缓释微丸在Beagle犬体内的药动学特征

发布时间：2018-03-07 14:06

本文选题：长春胺　切入点：pH依赖性　出处：《中国实验方剂学杂志》2015年03期 　论文类型：期刊论文

【摘要】：目的:制备长春胺缓释微丸并考察其在Beagle犬体内的药动学特征,为非p H依赖性释放的长春胺缓释制剂研发提供参考。方法:制备酒石酸丸芯,采用流化床混悬液上药法制备长春胺缓释微丸。Beagle犬随机分成2组,单剂量双周期交叉口服长春胺缓释微丸与普通片,采用HPLC测定血药浓度,流动相0.02 mol·L-1磷酸二氢钾-乙腈(70∶30,用磷酸调节p H2.3),检测波长268 nm,比较各制剂的药动学参数。结果:长春胺缓释微丸与普通片在Beagle犬血浆中Cmax分别为(1 147.40±554.50),(1 506.10±327.44)μg·L-1;Tmax分别为(2.38±0.25),(1.63±0.25)h;MRT分别为(6.75±2.44),(3.19±0.73)h;AUC0-t分别为(4 766.76±1 740.26),(3 906.81±686.53)μg·h·L-1。长春胺缓释微丸较普通片的相对生物利用度122%,体内外相关性良好。结论:与普通片相比,长春胺缓释微丸在Beagle犬体内吸收较慢,平均滞留时间为普通片的2倍以上,生物利用度显著提高,说明该处方可实现药物在胃肠道中非p H依赖性释放。
[Abstract]:Objective: to prepare vincristine sustained-release pellets and investigate its pharmacokinetic characteristics in Beagle dogs. Vincristine sustained-release pellets. Beagle dogs were prepared by fluidized bed suspension method. They were randomly divided into two groups. Vincristine sustained-release pellets and common tablets were taken at a single dose and double cycle intersection. The concentration of vincristine in blood was determined by HPLC. The mobile phase 0.02 mol 路L -1 potassium dihydrogen phosphate-acetonitrile 70: 30, adjusted with phosphoric acid and detected at 268 nm, was used to compare the pharmacokinetic parameters of each preparation. Results: the Cmax values of vincristine sustained-release pellets and common tablets in plasma of Beagle dogs were 1.147.40 卤554.506.10 卤327.44) 渭 g 路L ~ (-1) T _ (max) were 2.38 卤0.250.63 卤0.25hmh ~ (-1) 渭 g 路L ~ (-1), respectively. AUC 0-t was 4 766.76. 76. 76. 76 卤1 740.26) 渭 g 路h 路L -1. The relative bioavailability of vincristine sustained-release pellets was better than that of common tablets. Conclusion: compared with ordinary tablets, the relative bioavailability of vincristine sustained-release pellets is better than that of common tablets in vivo and in vitro. The absorption of vincristine sustained-release pellets in Beagle dogs was slow, the average retention time was more than 2 times of that of common tablets, and the bioavailability was significantly increased, which indicated that the formulation could realize the release of non-H dependent drugs in gastrointestinal tract.
【作者单位】：大连大学;上海市计划生育科学研究所国家人口和计划生育委员会计划生育药具重点实验室上海生殖健康药具工程技术研究中心;上海中医药大学;
【分类号】：R96

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